Nearly every part of A. altissima has some application in Chinese traditional medicine. One of the oldest recipes, recorded in a work from 732 AD, is used for treating mental illness. It involved chopped root material, young boys' urine and douchi. After sitting for a day the liquid was strained out and given to the patient over the course of several days.

Another source from 684 AD, during the Tang dynasty and recorded in Li Shizhen's Compendium of Materia Medica, states that when the leaves are taken internally, they make one incoherent and sleepy, while when used externally they can be effectively used to treat boils, abscesses and itches. Yet another recipe recorded by Li uses the leaves to treat baldness. This formula calls for young leaves of ailanthus, catalpa and peach tree to be crushed together and the resulting liquid applied to the scalp to stimulate hair growth.

The dried bark, however, is still an officinal drug and is listed in the modern Chinese materia medica as chun bai pi (Chinese: 椿白皮; pinyin: chūnbáipí), meaning "white bark of spring". Modern works treat it in detail, discussing chemical constituents, how to identify the product and its pharmaceutical uses. It is prepared by felling the tree in fall or spring, stripping the bark and then scraping off the hardest, outermost portion, which is then sun-dried, soaked in water, partially re-dried in a basket and finally cut into strips. The bark is said to have cooling and astringent properties and is primarily used to treat dysentery, intestinal hemorrhage, menorrhagia and spermatorrhea. It is only prescribed in amounts between 4 and 10 grams, so as not to poison the patients. Li's Compendium has 18 recipes that call for the bark. Asian and European chemists have found some justification for its medical use as it contains a long list of active chemicals that include quassin and saponin, while ailanthone, the allelopathic chemical in the tree of heaven, is a known antimalarial agent.It is available in most shops dealing in Chinese traditional medicine. A tincture of the root-bark has been used successfully in treating cardiac palpitation, asthma and epilepsy.

Anecdotal evidence suggests that the plant may be mildly toxic. The noxious odours have been associated with nausea and headaches, as well as with contact dermatitis reported in both humans and sheep, who also developed weakness and paralysis. It contains a quinone irritant, 2,6-dimethoxybenzoquinone, as well as active quassinoids (ailanthone itself being one) which may account for these effects, but they have, however, proved difficult or impossible to reproduce in humans and goats. In one trial a tincture from the blossom and foliage caused nausea, vomiting and muscular relaxation.